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BAR501是高效选择性的 GPBAR1激动剂(EC50:1 μM)。


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BAR501是高效选择性的 GPBAR1激动剂(EC50:1 μM)。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 289 | In stock | |
| 5 mg | ¥ 629 | In stock | |
| 10 mg | ¥ 1,060 | In stock | |
| 25 mg | ¥ 2,230 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 763 | In stock |
BAR501 相关产品
| 产品描述 | BAR501 is an effective and specific GPBAR1 agonist (EC50: 1 μM). |
| 靶点活性 | GPBAR1:1 μM(EC50) |
| 体外活性 | In HEK293 cells overexpressing a CRE along with GPBAR1, BAR501 effectively transactivates GPBAR1 (EC50: 1 μM). In GLUTAg cells, BAR501 (10 μM) increases the mRNA expression of GLP-1 by 2.5 folds. |
| 体内活性 | Pretreating rats for 6 days with BAR501 (15 mg/kg), the basal portal pressure reduces and the vasoconstriction activity of norepinephrine blunts. BAR501 attenuates the hepatic vasomotor activity induced by methoxamine and shear stress. In the CCl4 model, BAR501 exerts a direct vasodilatory activity. BAR501 (15 mg/kg) can reduce AST plasma levels and portal pressure. BAR501 attenuates endothelial dysfunction by regulating CSE expression/activity. |
| 细胞实验 | For GPBAR1 mediated transactivation, HEK-293T cells are plated at 10000 cells/well in a 24 well-plate and transfected with 200 ng of pGL4.29, a reporter vector containing a cAMP response element (CRE) that drives the transcription of the luciferase reporter gene luc2P, with 100 ng of pCMVSPORT6-human GPBAR1, and with 100 ng of pGL4.70. At 24 h post-transfection, HepG2 and HEK293T cells are incubated with 10 μM BAR501 for 18 h and luciferase activities are assayed and normalized against the Renilla activities[1]. |
| 动物实验 | Animal: C57BL6 miceAdministration: i.p., 500 μL/kg of CCl4 in an equal volume of paraffin oil twice a week for 9 weeks. CCL4 mice are randomized to receive BAR501 (15 mg/Kg daily by gavage) or vehicle (distilled water). Serum bilirubin, albumin, aspartate aminotransferase, alanine aminotransferase and alkaline phosphatase are measured by routine biochemical clinical chemistry[1]. |
| 别名 | BAR 501 |
| 分子量 | 406.64 |
| 分子式 | C26H46O3 |
| CAS No. | 1632118-69-4 |
| Smiles | CC[C@@H]1[C@H](O)[C@H]2[C@@H]3CC[C@H]([C@H](C)CCCO)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 |
| 密度 | 1.047 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 50 mg/mL (122.96 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
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DMSO
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